Výsledky vyhledávání - "Scot Richard Mente"

Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor

Autor: Dmitri Volfson, Rebecca E. O’Connor, Ivan Viktorovich Efremov, Michael D. Ehlers, Scot Richard Mente, John A. Allen, Rouba Kozak, Edward Guilmette, George J DeMarco, Patrick L. Tierney, David Gray, Jennifer Elizabeth Davoren, Michelle A. Salafia

Publikováno v: Nature Communications, Vol 9, Iss 1, Pp 1-17 (2018)
Nature Communications

Selective activation of dopamine D1 receptors (D1Rs) has been pursued for 40 years as a therapeutic strategy for neurologic and psychiatric diseases due to the fundamental role of D1Rs in motor function, reward processing, and cognition. All known D1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9abee3005f246813ed027c3eb3d448ae
http://link.springer.com/article/10.1038/s41467-017-02776-7

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Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors

Autor: Angela C. Doran, Cheng Chang, Shenping Liu, Butler Todd W, Travis T. Wager, Klaas Schildknegt, Lei Zhang, Michael Marconi, Jianke Li, Scot Richard Mente, Katherine Fisher, Ramalakshmi Yegna Chandrasekaran, Joseph R. Hedde, Sarah Grimwood, Chakrapani Subramanyam, Paul Galatsis

Publikováno v: ACS Chemical Neuroscience. 8:1995-2004

To enable the clinical development of our CNS casein kinase 1 delta/epsilon (CK1δ/e) inhibitor project, we investigated the possibility of developing a CNS positron emission tomography (PET) radioligand. For this effort, we focused our design and sy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4c7a24bb9dc9c4035e136f3bff24189
https://doi.org/10.1021/acschemneuro.7b00155

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Potent α-Synuclein Aggregation Inhibitors, Identified by High-Throughput Screening, Mainly Target the Monomeric State

Autor: Christian Moestrup Jessen, Keith Pitts, Hossein Mohammad-Beigi, Martin Kurnik, Nikolai Lorenzen, Roland G.W. Staal, Cagla Sahin, Daniel E. Otzen, Scot Richard Mente, Frans A. A. Mulder, Jan Skov Pedersen, Camilla Bertel Andersen, Lise Giehm, Warren D. Hirst, Girija Krishnamurthy, Gunna Christiansen, Peter H. Reinhart, Steen V. Petersen

Publikováno v: Kurnik, M, Sahin, C, Andersen, C B, Lorenzen, N, Giehm, L, Mohammad-Beigi, H, Jessen, C M, Pedersen, J S, Christiansen, G, Petersen, S V, Staal, R, Krishnamurthy, G, Pitts, K, Reinhart, P H, Mulder, F A A, Mente, S, Hirst, W D & Otzen, D E 2018, ' Potent α-Synuclein Aggregation Inhibitors, Identified by High-Throughput Screening, Mainly Target the Monomeric State ', Cell Chemical Biology, vol. 25, no. 11, pp. 1389-1402 . https://doi.org/10.1016/j.chembiol.2018.08.005

α-Synuclein (αSN) aggregation is central to the etiology of Parkinson's disease (PD). Large-scale screening of compounds to identify aggregation inhibitors is challenged by stochastic αSN aggregation and difficulties in detecting early-stage oligo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d6e9912e43fa58913d068c4c4085319
https://pure.au.dk/portal/da/publications/potent-synuclein-aggregation-inhibitors-identified-by-highthroughput-screening-mainly-target-the-monomeric-state(5db8c797-9129-4ffc-9d50-99cacae6acc6).html

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Mapping the binding site of BMS-708163 on γ-secretase with cleavable photoprobes

Autor: Natalya Gertsik, Uthpala Seneviratne, Chuong Nguyen, Paramita Mukherjee, Yue-Ming Li, Christopher W. am Ende, Scot Richard Mente, Douglas S. Johnson, Kieran F. Geoghegan

γ-Secretase, a four-subunit transmembrane aspartic proteinase, is a highly valued drug target in Alzheimer's disease and cancer. Despite significant progress in structural studies, the respective molecular mechanisms and binding modes of γ-secretas

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15738c76f005cbca647de075a4dfd989
https://europepmc.org/articles/PMC5516958/

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The Use of the R Language for Medicinal Chemistry Applications

Autor: Scot Richard Mente, Max Kuhn

Publikováno v: Current Topics in Medicinal Chemistry. 12:1957-1964

This manuscript serves as a review of how the R language has been used in the last decade to address problems related to medicinal chemistry design. This includes the use of the R language for chemoinformatics applications and interfaces, as well as

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c785c39bc772e9b67849c3f6b386fc11
https://doi.org/10.2174/1568026611212180003

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Exploring Aromatic Chemical Space with NEAT: Novel and Electronically Equivalent Aromatic Template

Autor: Jeffrey A. Pfefferkorn, Alan M. Mathiowetz, Angel Guzman-Perez, Matthew Merrill Hayward, Brajesh K. Rai, John William Benbow, Cristiano Ruch Werneck Guimarães, Scot Richard Mente, Spiros Liras, Mary Theresa Didiuk, Meihua Tu

Publikováno v: Journal of Chemical Information and Modeling. 52:1114-1123

In this paper, we describe a lead transformation tool, NEAT (Novel and Electronically equivalent Aromatic Template), which can help identify novel aromatic rings that are estimated to have similar electrostatic potentials, dipoles, and hydrogen bondi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::51b66b69942ffe7cb320ba69472f0fff
https://doi.org/10.1021/ci300031s

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